JP2004516311A - アトルバスタチン結晶体 - Google Patents
アトルバスタチン結晶体 Download PDFInfo
- Publication number
- JP2004516311A JP2004516311A JP2002552901A JP2002552901A JP2004516311A JP 2004516311 A JP2004516311 A JP 2004516311A JP 2002552901 A JP2002552901 A JP 2002552901A JP 2002552901 A JP2002552901 A JP 2002552901A JP 2004516311 A JP2004516311 A JP 2004516311A
- Authority
- JP
- Japan
- Prior art keywords
- intensity
- polymorph
- crystalline polymorph
- atorvastatin
- phenylamino
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 239000013078 crystal Substances 0.000 title claims abstract description 76
- XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 title description 7
- XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 title description 7
- 229960005370 atorvastatin Drugs 0.000 title description 7
- OJRHUICOVVSGSY-RXMQYKEDSA-N (2s)-2-chloro-3-methylbutan-1-ol Chemical compound CC(C)[C@H](Cl)CO OJRHUICOVVSGSY-RXMQYKEDSA-N 0.000 claims abstract description 39
- 229960001770 atorvastatin calcium Drugs 0.000 claims abstract description 33
- 238000004519 manufacturing process Methods 0.000 claims abstract description 20
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 4
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 28
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims description 27
- 238000010586 diagram Methods 0.000 claims description 24
- 239000000725 suspension Substances 0.000 claims description 24
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 23
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 23
- 239000000203 mixture Substances 0.000 claims description 17
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 15
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 15
- 239000003960 organic solvent Substances 0.000 claims description 15
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 14
- WPPHUTKYAGKEJJ-UHFFFAOYSA-L calcium;7-pyrrol-1-ylheptanoate Chemical compound [Ca+2].[O-]C(=O)CCCCCCN1C=CC=C1.[O-]C(=O)CCCCCCN1C=CC=C1 WPPHUTKYAGKEJJ-UHFFFAOYSA-L 0.000 claims description 14
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 14
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 14
- 239000002904 solvent Substances 0.000 claims description 10
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 9
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 7
- OUCSEDFVYPBLLF-KAYWLYCHSA-N 5-(4-fluorophenyl)-1-[2-[(2r,4r)-4-hydroxy-6-oxooxan-2-yl]ethyl]-n,4-diphenyl-2-propan-2-ylpyrrole-3-carboxamide Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@H]2OC(=O)C[C@H](O)C2)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 OUCSEDFVYPBLLF-KAYWLYCHSA-N 0.000 claims description 6
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 claims description 5
- 238000001035 drying Methods 0.000 claims description 5
- 238000001704 evaporation Methods 0.000 claims description 3
- AXCZMVOFGPJBDE-UHFFFAOYSA-L calcium dihydroxide Chemical compound [OH-].[OH-].[Ca+2] AXCZMVOFGPJBDE-UHFFFAOYSA-L 0.000 claims description 2
- 239000000920 calcium hydroxide Substances 0.000 claims description 2
- 229910001861 calcium hydroxide Inorganic materials 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 238000002360 preparation method Methods 0.000 description 10
- 239000000243 solution Substances 0.000 description 10
- 230000001747 exhibiting effect Effects 0.000 description 7
- 238000001914 filtration Methods 0.000 description 7
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 6
- 238000003756 stirring Methods 0.000 description 6
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 description 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 238000000113 differential scanning calorimetry Methods 0.000 description 3
- 230000008018 melting Effects 0.000 description 3
- 238000002844 melting Methods 0.000 description 3
- 239000007787 solid Substances 0.000 description 3
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 3
- 0 CC(C)c1c(*=O)c(C2C=CC=CC2)c(-c(cc2)ccc2F)[n]1CCC(CC(CC(O)=O)=O)=O Chemical compound CC(C)c1c(*=O)c(C2C=CC=CC2)c(-c(cc2)ccc2F)[n]1CCC(CC(CC(O)=O)=O)=O 0.000 description 2
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 2
- 150000003863 ammonium salts Chemical class 0.000 description 2
- -1 atorvastatin ammonium salt Chemical class 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- 159000000007 calcium salts Chemical class 0.000 description 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 2
- 238000011067 equilibration Methods 0.000 description 2
- 229910052757 nitrogen Inorganic materials 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 1
- PAYRUJLWNCNPSJ-UHFFFAOYSA-N Nc1ccccc1 Chemical compound Nc1ccccc1 PAYRUJLWNCNPSJ-UHFFFAOYSA-N 0.000 description 1
- 238000002441 X-ray diffraction Methods 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000012267 brine Substances 0.000 description 1
- XQKKWWCELHKGKB-UHFFFAOYSA-L calcium acetate monohydrate Chemical compound O.[Ca+2].CC([O-])=O.CC([O-])=O XQKKWWCELHKGKB-UHFFFAOYSA-L 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- AQEFLFZSWDEAIP-UHFFFAOYSA-N di-tert-butyl ether Chemical compound CC(C)(C)OC(C)(C)C AQEFLFZSWDEAIP-UHFFFAOYSA-N 0.000 description 1
- 150000002009 diols Chemical class 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- LMBMDLOSPKIWAP-UHFFFAOYSA-N embutramide Chemical compound OCCCC(=O)NCC(CC)(CC)C1=CC=CC(OC)=C1 LMBMDLOSPKIWAP-UHFFFAOYSA-N 0.000 description 1
- 150000002170 ethers Chemical class 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 239000006260 foam Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- 230000002440 hepatic effect Effects 0.000 description 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 description 1
- 150000002596 lactones Chemical class 0.000 description 1
- 229910052943 magnesium sulfate Inorganic materials 0.000 description 1
- 235000019341 magnesium sulphate Nutrition 0.000 description 1
- 230000001603 reducing effect Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- VVRPOCPLIUDBSA-CNZCJKERSA-M sodium;(3r,5r)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-propan-2-ylpyrrol-1-yl]-3,5-dihydroxyheptanoate Chemical compound [Na+].C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC([O-])=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 VVRPOCPLIUDBSA-CNZCJKERSA-M 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 238000000935 solvent evaporation Methods 0.000 description 1
- 239000011877 solvent mixture Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000007966 viscous suspension Substances 0.000 description 1
Images
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pyrrole Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP00811249 | 2000-12-27 | ||
PCT/EP2001/015012 WO2002051804A1 (fr) | 2000-12-27 | 2001-12-19 | Formes cristallines d'atorvastatine |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009127757A Division JP2009221216A (ja) | 2000-12-27 | 2009-05-27 | アトルバスタチン結晶体 |
Publications (1)
Publication Number | Publication Date |
---|---|
JP2004516311A true JP2004516311A (ja) | 2004-06-03 |
Family
ID=8175112
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2002552901A Withdrawn JP2004516311A (ja) | 2000-12-27 | 2001-12-19 | アトルバスタチン結晶体 |
JP2009127757A Pending JP2009221216A (ja) | 2000-12-27 | 2009-05-27 | アトルバスタチン結晶体 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009127757A Pending JP2009221216A (ja) | 2000-12-27 | 2009-05-27 | アトルバスタチン結晶体 |
Country Status (23)
Country | Link |
---|---|
US (4) | US7538136B2 (fr) |
EP (2) | EP2000461A1 (fr) |
JP (2) | JP2004516311A (fr) |
KR (1) | KR100790766B1 (fr) |
CN (1) | CN1273449C (fr) |
AT (1) | ATE420070T1 (fr) |
AU (1) | AU2002224952B2 (fr) |
CA (7) | CA2622477A1 (fr) |
CZ (1) | CZ20032019A3 (fr) |
DE (1) | DE60137364D1 (fr) |
ES (1) | ES2319870T3 (fr) |
HR (1) | HRP20030607A2 (fr) |
HU (1) | HUP0302519A3 (fr) |
IL (1) | IL156280A0 (fr) |
IS (1) | IS6859A (fr) |
MX (1) | MXPA03005879A (fr) |
NO (1) | NO20032758D0 (fr) |
NZ (1) | NZ527048A (fr) |
PL (1) | PL365312A1 (fr) |
PT (1) | PT1345896E (fr) |
SK (1) | SK9532003A3 (fr) |
WO (1) | WO2002051804A1 (fr) |
ZA (1) | ZA200304297B (fr) |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2008007507A (ja) * | 2006-06-28 | 2008-01-17 | Teva Pharmaceutical Industries Ltd | 結晶形アトルバスタチン |
JP2008534669A (ja) * | 2005-04-08 | 2008-08-28 | エギシュ ヂョヂセルヂャール ニルヴァーノサン ミケデ レースヴェーニタールササーグ | 新規な結晶性のアトルバスタチンヘミカルシウム塩の多形相 |
JP2012031130A (ja) * | 2010-07-28 | 2012-02-16 | Kyongbo Pharm Co Ltd | アトルバスタチンヘミカルシウム塩の新規な結晶形、その水和物、及びその製造方法 |
WO2018008569A1 (fr) * | 2016-07-04 | 2018-01-11 | ゼリア新薬工業株式会社 | Procédé de production de sel de calcium de composé 1, 5-benzodiazépine |
Families Citing this family (33)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7411075B1 (en) | 2000-11-16 | 2008-08-12 | Teva Pharmaceutical Industries Ltd. | Polymorphic form of atorvastatin calcium |
CA2426632C (fr) * | 2000-11-03 | 2008-08-05 | Teva Pharmaceutical Industries, Ltd. | Atorvastatine hemicalcique forme vii |
IL156055A0 (en) * | 2000-11-30 | 2003-12-23 | Teva Pharma | Novel crystal forms of atorvastatin hemi calcium and processes for their preparation as well as novel processes for preparing other forms |
US7501450B2 (en) * | 2000-11-30 | 2009-03-10 | Teva Pharaceutical Industries Ltd. | Crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms |
ATE420070T1 (de) * | 2000-12-27 | 2009-01-15 | Teva Pharma | Kristalline formen von atorvastatin |
EE200300597A (et) * | 2001-06-29 | 2004-02-16 | Warner-Lambert Company Llc | [R-(R*,R*)]-2-(4-fluorofenüül)-beeta, delta-dihüdroksü-5-(1-metüületüül)-3-fenüül-4-[fenüülamino)karbonüül]-1H-pürrool-1-hepta anhappe kaltsiumsoola (2:1) (atorvastatiini) kristallilised vormid |
US7074818B2 (en) | 2001-07-30 | 2006-07-11 | Dr. Reddy's Laboratories Limited | Crystalline forms VI and VII of Atorvastatin calcium |
CZ2004126A3 (cs) * | 2001-07-30 | 2004-12-15 | Dr. Reddy's Laboratories Limited | Krystalické formy VI. A VII. vápenaté soli atorvastatinu |
AU2002324715B2 (en) * | 2001-08-16 | 2009-03-12 | Teva Pharmaceutical Industries Ltd. | Processes for preparing calcium salt forms of statins |
CA2456095C (fr) * | 2001-08-31 | 2010-05-11 | Morepen Laboratories Ltd. | Procede ameliore de preparation d'un sel d'atorvastatine calcique amorphe (2:1) |
UA77990C2 (en) * | 2001-12-12 | 2007-02-15 | Crystalline calcium salt of (2:1) [r-(r*,r*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1h-pyrroleheptanic acid | |
DE03713610T1 (de) * | 2002-02-15 | 2005-10-20 | Teva Pharma | Neue kristallformen von atorvastatin-hemicalcium und verfahren zu deren herstellung, sowie neue verfahren zur herstellung der formen i, viii und ix von atorvastatin-hemicalcium |
IL163594A0 (en) | 2002-02-19 | 2005-12-18 | Teva Pharma | Processes for desolvating solvates of atorvastatinhemi-calcium and atorvastatin hemi-calcium essentially free of organic solvent |
EP1562583A1 (fr) * | 2002-09-03 | 2005-08-17 | Morepen Laboratories Ltd. | Forme vi de calcium d'atorvastatine ou hydrates de cette derniere |
AU2003297594A1 (en) * | 2002-11-28 | 2004-06-23 | Teva Pharmaceutical Industries Ltd. | Crystalline form f of atorvastatin hemi-calcium salt |
EP1424324A1 (fr) * | 2002-11-28 | 2004-06-02 | Teva Pharmaceutical Industries Limited | Forme cristalline F de calcium d'atorvastatine |
US20050271717A1 (en) | 2003-06-12 | 2005-12-08 | Alfred Berchielli | Pharmaceutical compositions of atorvastatin |
US7655692B2 (en) | 2003-06-12 | 2010-02-02 | Pfizer Inc. | Process for forming amorphous atorvastatin |
CA2627940A1 (fr) | 2004-03-17 | 2005-10-06 | Ranbaxy Laboratories Limited | Procede de production d'atorvastatine calcique sous forme amorphe |
EP1761489A1 (fr) * | 2004-03-17 | 2007-03-14 | Ranbaxy Laboratories Limited | Forme cristalline d'hemi-calcium d'atorvastatine |
EP1745020A2 (fr) | 2004-05-05 | 2007-01-24 | Pfizer Products Incorporated | Formes salines d'acide ¬r-(r*, r*)|-2-(4-fluorophenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-¬(phenylamino)carbonyl|-1h-pyrrole-1-heptanoique |
JP4915919B2 (ja) | 2004-06-11 | 2012-04-11 | Sbiバイオテック株式会社 | インターフェロン産生細胞の活性調節剤 |
JP5000502B2 (ja) * | 2004-07-16 | 2012-08-15 | レツク・フアーマシユーテイカルズ・デー・デー | アトルバスタチンカルシウムの酸化分解生成物 |
CA2573771C (fr) | 2004-07-20 | 2011-05-10 | Warner-Lambert Company Llc | Nouvelles formes de sel de calcium (2:1) d'acide [r-(r*,r*)]-2-(4-fluorophenyl)-.beta., .gamma.-dihydroxy-5-(1-menthylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1h-pyrrole-1-heptanoique |
BRPI0519996A2 (pt) | 2004-10-28 | 2009-04-07 | Warner Lambert Co | processo para formar atorvastatina amorfa |
WO2006048894A1 (fr) * | 2004-11-05 | 2006-05-11 | Morepen Laboratories Limited | Nouvelles formes cristallines de calcium d'atorvastatine et procedes de fabrication |
CA2499047A1 (fr) * | 2005-03-01 | 2006-09-01 | Apotex Pharmachem Inc. | Methode de synthese d'un sel de semi-calcium d'atorvastatine |
CA2547216A1 (fr) | 2005-09-21 | 2007-03-21 | Renuka D. Reddy | Procede de recuit de l'atorvastatine amorphe |
DE602006014193D1 (de) | 2005-11-21 | 2010-06-17 | Warner Lambert Co | Neue formen von är-(r*,r*)ü-2-(4-fluorphenyl)-b,d-dihydroxy-5-(1-methylethyl)-3-phenyl-4-ä(phenylamino)carbonylü-1h-pyrrol-1-heptansäure-magnesium |
KR20100023059A (ko) | 2005-12-13 | 2010-03-03 | 테바 파마슈티컬 인더스트리즈 리미티드 | 아토바스타틴 헤미칼슘의 결정형 및 이의 제조 방법 |
EP1810667A1 (fr) | 2006-01-20 | 2007-07-25 | KRKA, tovarna zdravil, d.d., Novo mesto | Composition pharmaceutique contenant de l'atorvastatin amorphé |
EP2185527A2 (fr) * | 2007-07-11 | 2010-05-19 | Actavis Group PTC EHF | Nouveau polymorphe d'atorvastatine calcium et son utilisation pour la préparation d'atorvastatine calcium amorphe |
CN104983702A (zh) * | 2015-07-23 | 2015-10-21 | 青岛蓝盛洋医药生物科技有限责任公司 | 一种治疗高胆固醇血症的药物阿托伐他汀钙组合物片剂 |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FI94339C (fi) * | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
DK0680320T3 (da) * | 1993-01-19 | 1999-10-25 | Warner Lambert Co | Stabilt oralt CI-981-præparat og fremgangsmåde til fremstilling deraf |
US5298627A (en) * | 1993-03-03 | 1994-03-29 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
HRP960313B1 (en) * | 1995-07-17 | 2002-08-31 | Warner Lambert Co | Form iii crystalline (r- (r*, r*)-2- (4-fluorophenyl) -beta-delta-hydroxy-5-(1-methylethyl) -3-phenyl-4- ((phenylamino) carbonyl -1h-pyrrole-1-heptanoic acid calcium salt (2:1) |
HRP960312B1 (en) | 1995-07-17 | 2001-10-31 | Warner Lambert Co | NOVEL PROCESS FOR THE PRODUCTION OF AMORPHOUS /R-(R*, R*)/-2-(4-FLUOROPHENYL)-"beta", "delta"-DIHYDROXY-5-PHENYL-4-/(PHENYLAMINO)CARBONYL/-1H-PYRROLE -1-HEPTANOIC ACID CALCIUM SALT (2 : 1) |
WO1997003959A1 (fr) * | 1995-07-17 | 1997-02-06 | Warner-Lambert Company | Formes cristallines d'hemi-sel de calcium d'acide [r-(r*,r*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1h-pyrrole-1-heptanoique (atorvastatine) |
US7411075B1 (en) * | 2000-11-16 | 2008-08-12 | Teva Pharmaceutical Industries Ltd. | Polymorphic form of atorvastatin calcium |
YU35802A (sh) | 1999-11-17 | 2005-07-19 | Teva Pharmaceutical Industries Ltd. | Polimorfni oblik atorvastatin kalcijuma |
DE60026737T2 (de) * | 1999-12-17 | 2006-09-21 | Pfizer Science And Technology Ireland Ltd., Dun Laoghaire | Verfahren zur herstellung von kristallin atorvastin kalcium |
CA2426632C (fr) * | 2000-11-03 | 2008-08-05 | Teva Pharmaceutical Industries, Ltd. | Atorvastatine hemicalcique forme vii |
IL156055A0 (en) * | 2000-11-30 | 2003-12-23 | Teva Pharma | Novel crystal forms of atorvastatin hemi calcium and processes for their preparation as well as novel processes for preparing other forms |
ATE420070T1 (de) * | 2000-12-27 | 2009-01-15 | Teva Pharma | Kristalline formen von atorvastatin |
WO2002057228A1 (fr) | 2001-01-17 | 2002-07-25 | Biocon India Limited | Atorvastatine calcique |
WO2002057229A1 (fr) * | 2001-01-19 | 2002-07-25 | Biocon India Limited | FORME V CRISTALLINE DE SEL HEMICALCIQUE D'ACIDE [R-(R*,R*)]-2-(4-FLUOROPHENYL)-ß,$G(D)-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1-HEPTANOIQUE (ATORVASTATINE) |
SI20814A (sl) | 2001-01-23 | 2002-08-31 | LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. | Priprava amorfnega atorvastatina |
SI20848A (sl) | 2001-03-14 | 2002-10-31 | Lek, Tovarna Farmacevtskih In Kemijskih Izdelkov, D.D. | Farmacevtska formulacija, ki vsebuje atorvastatin kalcij |
EE200300597A (et) * | 2001-06-29 | 2004-02-16 | Warner-Lambert Company Llc | [R-(R*,R*)]-2-(4-fluorofenüül)-beeta, delta-dihüdroksü-5-(1-metüületüül)-3-fenüül-4-[fenüülamino)karbonüül]-1H-pürrool-1-hepta anhappe kaltsiumsoola (2:1) (atorvastatiini) kristallilised vormid |
CZ2004126A3 (cs) * | 2001-07-30 | 2004-12-15 | Dr. Reddy's Laboratories Limited | Krystalické formy VI. A VII. vápenaté soli atorvastatinu |
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2001
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- 2001-12-19 CA CA002622477A patent/CA2622477A1/fr not_active Abandoned
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- 2001-12-19 WO PCT/EP2001/015012 patent/WO2002051804A1/fr active IP Right Grant
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2008534669A (ja) * | 2005-04-08 | 2008-08-28 | エギシュ ヂョヂセルヂャール ニルヴァーノサン ミケデ レースヴェーニタールササーグ | 新規な結晶性のアトルバスタチンヘミカルシウム塩の多形相 |
JP2008007507A (ja) * | 2006-06-28 | 2008-01-17 | Teva Pharmaceutical Industries Ltd | 結晶形アトルバスタチン |
JP2012031130A (ja) * | 2010-07-28 | 2012-02-16 | Kyongbo Pharm Co Ltd | アトルバスタチンヘミカルシウム塩の新規な結晶形、その水和物、及びその製造方法 |
WO2018008569A1 (fr) * | 2016-07-04 | 2018-01-11 | ゼリア新薬工業株式会社 | Procédé de production de sel de calcium de composé 1, 5-benzodiazépine |
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